ABSTRACT The major goal of the proposed research is to design and utilize novel catalytic C-H bond activation methods for the synthesis of complex organic compounds of phamaceutical importance. The first aim of the project is to develop and utilize the catalytic C-H coupling methods to synthesize a number of biologically active target molecules, including tamoxifen, celivarone and sulindac. The second aim of the project incorporates catalytic coupling method of amino acid derivatives via C-N bond cleavage to synthesize a number of complex molecules of pharmaceutical importance, including donepezil and STX-1040. The proposed research plan aims to develop novel catalytic coupling methods to synthesize a variety of high-value target molecules with potent anticancer and anti-inflammatory biological activities under environmentally sustainable conditions. The project seeks financial support of one postdoctoral associate and one graduate student to carry out the proposed project.